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Previous studies have demonstrated that synaptic AMPARs
2023-09-12
Previous studies have demonstrated that synaptic AMPARs can differ greatly in their mobility; some rapidly and constitutively OICR-9429 in and out of the synaptic membrane, while others remain somewhat stable in the synaptic membrane (Luscher et al., 1999, Luthi et al., 1999). We find that mGluR- a
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The aldehyde reductase AKR A
2023-09-12
The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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Norepinephrine and epinephrine are catecholamines
2023-09-12
Norepinephrine and epinephrine are catecholamines (CA) released from synaptic nerves and the adrenal gland that mediate systemic responses to nutritional stressors (Cannon and De la Paz, 1911). CA mobilize plasma glucose by suppressing insulin secretion from the pancreatic β-cell (Katada and Ui, 198
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Our previous work fails to show any maternal
2023-09-12
Our previous work fails to show any maternal effect with blockade of 5-HT2A receptor, as acute and repeated treatment of MDL100907 does not alter maternal behavior at the behaviorally active doses (Chen et al., 2014). In the present study, MDL100907 pretreatment attenuated the maternal disruptive ef
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opioid receptors In the previous study we demonstrated the i
2023-09-12
In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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SKF 81297 hydrobromide Endogenous adenosine systems have lar
2023-09-12
Endogenous adenosine systems have largely been implicated in drug actions by the demonstration that caffeine (non-selective A1R and A2AR antagonist) (see Section The issue of caffeine), in doses up to 7.5–10mg/kg, inhibits antinociception, and when this occurs, it SKF 81297 hydrobromide is generall
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The syntheses of a and b are
2023-09-12
The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each DMPO yielded th
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Because of its role in
2023-09-12
Because of its role in tumor growth, proliferation and metastasis, Axl is considered a therapeutic target. Several Axl inhibitors, including low-molecular-weight agents and antibodies, have been reported. Axl inhibition, using low-molecular-weight inhibitors or shRNA knockdown, resulted in reduced t
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It has been shown that ACLY is
2023-09-12
It has been shown that ACLY is localized to not only the cytoplasm but also the nucleus. Nuclear ACLY may supply acetyl-CoA for histone acetylation, leading to global regulation of the gene expression [16], [18]. We previously reported that AZ2 is also localized to both the cytoplasm and nucleus whe
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FDA-approved Drug Library Somatostatin analogs also bind to
2023-09-12
Somatostatin analogs also bind to somatostatin receptors. It has been reported that octreotide has a high affinity for hSSTR2, moderate affinity for hSSTR3 and hSSTR5, and does not bind to hSSTR1 or hSSTR4 (Ben-Shlomo and Melmed 2008). Compared to octreotide, pasireotide displays 40-, 30-, and 5-fol
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HMGN proteins are subject to extensive
2023-09-12
HMGN proteins are subject to extensive post-translational modifications which influence both their mode of binding to Lonafarnib and their functional activity. Like the other HMG protein families, HMGNs are substrates for many of the same enzymes that modify histone proteins (review in [175]). The
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br Economics consequences of antibiotic resistance in
2023-09-11
Economics consequences of antibiotic resistance in a SICU In the era of cost-containment, surgeons also need to consider the economic impact of antibiotic resistance in the surgical patient. Antibiotic-resistant infections are more difficult to treat, are more costly and more likely to be fatal t
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Monastrol Sorafenib was the first small RTK inhibitor drug t
2023-09-11
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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br Transparency document br Introduction G protein
2023-09-11
Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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Extracellular ATP and downstream purinergic signaling have a
2023-09-11
Extracellular ATP and downstream purinergic signaling have also been proposed to contribute to dental pulp tissue healing and dentin regeneration. Mechanical and thermal stimulation of external dentin can induce ATP release in dental pulp through pannexins [13]. Cold stimulation was also reported to
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